The switch from antipsychotic to aripiprazole can be challenging, as the classical receptor theory predicts that the intrinsic activity of partial agonists is altered when the density of target receptors is modified. Therefore, we hypothesized that the partial agonist properties of aripiprazole would be more easily revealed on hypersensitive rat striatal tissues. A model of chronic treatments of rodents with typical antipsychotics, known to lead to an up-regulation and a hypersensitivity of dopamine D₂ receptors was used. Therefore, the functional response to aripiprazole and other full and partial agonists, obtained by [³⁵S]GTPgS binding was compared in striatal membranes from naïve rats or those exposed for three weeks to haloperidol. Experiments were performed in classical binding conditions, and in conditions known to facilitate the detection of the functional responses to low intrinsic activity partial agonists (the substitution of NaCl by NMDG). The partial agonist properties of aripiprazole were not revealed in different binding conditions, either on naïve nor hypersensitized striatal rat membranes. However, changing the binding conditions helped to detect the partial agonist profile of (-)-3-PPP, which was even enhanced on hypersensitized tissue. The difference observed between responses induced by full and partial agonists in distinct binding conditions could underline the functional selective profile at the level of the D₂ receptor. However, further experiments investigating the second-messenger cascades should be performed so as to establish the functional properties of aripiprazole and understand the mechanism underlying the switching issues in clinic.